IE48717B1 - A pharmaceutical preparation comprising a cardiac glycoside in combination with a polymer,and a process for preparation thereof - Google Patents
A pharmaceutical preparation comprising a cardiac glycoside in combination with a polymer,and a process for preparation thereofInfo
- Publication number
- IE48717B1 IE48717B1 IE245579A IE245579A IE48717B1 IE 48717 B1 IE48717 B1 IE 48717B1 IE 245579 A IE245579 A IE 245579A IE 245579 A IE245579 A IE 245579A IE 48717 B1 IE48717 B1 IE 48717B1
- Authority
- IE
- Ireland
- Prior art keywords
- preparation
- cardiac glycoside
- polymer
- layer
- cardiac
- Prior art date
Links
- 229940097217 cardiac glycoside Drugs 0.000 title claims abstract description 27
- 239000002368 cardiac glycoside Substances 0.000 title claims abstract description 27
- 229930002534 steroid glycoside Natural products 0.000 title claims abstract description 27
- 238000002360 preparation method Methods 0.000 title claims abstract description 24
- 229920000642 polymer Polymers 0.000 title claims abstract description 20
- LPMXVESGRSUGHW-HBYQJFLCSA-N ouabain Chemical compound O[C@@H]1[C@H](O)[C@@H](O)[C@H](C)O[C@H]1O[C@@H]1C[C@@]2(O)CC[C@H]3[C@@]4(O)CC[C@H](C=5COC(=O)C=5)[C@@]4(C)C[C@@H](O)[C@@H]3[C@@]2(CO)[C@H](O)C1 LPMXVESGRSUGHW-HBYQJFLCSA-N 0.000 title claims abstract description 18
- 239000000825 pharmaceutical preparation Substances 0.000 title claims abstract description 16
- 238000000034 method Methods 0.000 title claims abstract description 15
- 239000000463 material Substances 0.000 claims abstract description 8
- 238000005507 spraying Methods 0.000 claims abstract description 7
- 239000000203 mixture Substances 0.000 claims description 7
- 125000000129 anionic group Chemical group 0.000 claims description 5
- 239000012530 fluid Substances 0.000 claims description 5
- 238000004519 manufacturing process Methods 0.000 claims description 4
- 239000007787 solid Substances 0.000 claims description 3
- 239000002253 acid Substances 0.000 abstract description 4
- 210000002784 stomach Anatomy 0.000 abstract description 4
- 230000000747 cardiac effect Effects 0.000 abstract description 3
- 239000011248 coating agent Substances 0.000 abstract description 3
- 238000000576 coating method Methods 0.000 abstract description 3
- 239000002245 particle Substances 0.000 abstract 1
- 239000011162 core material Substances 0.000 description 13
- LTMHDMANZUZIPE-UHFFFAOYSA-N 3-[3-[5-[5-(4,5-dihydroxy-6-methyloxan-2-yl)oxy-4-hydroxy-6-methyloxan-2-yl]oxy-4-hydroxy-6-methyloxan-2-yl]oxy-12,14-dihydroxy-10,13-dimethyl-1,2,3,4,5,6,7,8,9,11,12,15,16,17-tetradecahydrocyclopenta[a]phenanthren-17-yl]-2h-furan-5-one Chemical compound C1C(O)C(O)C(C)OC1OC1C(C)OC(OC2C(OC(OC3CC4C(C5C(C6(CCC(C6(C)C(O)C5)C=5COC(=O)C=5)O)CC4)(C)CC3)CC2O)C)CC1O LTMHDMANZUZIPE-UHFFFAOYSA-N 0.000 description 9
- 150000008143 steroidal glycosides Chemical class 0.000 description 9
- 239000004480 active ingredient Substances 0.000 description 8
- LTMHDMANZUZIPE-AMTYYWEZSA-N Digoxin Natural products O([C@H]1[C@H](C)O[C@H](O[C@@H]2C[C@@H]3[C@@](C)([C@@H]4[C@H]([C@]5(O)[C@](C)([C@H](O)C4)[C@H](C4=CC(=O)OC4)CC5)CC3)CC2)C[C@@H]1O)[C@H]1O[C@H](C)[C@@H](O[C@H]2O[C@@H](C)[C@H](O)[C@@H](O)C2)[C@@H](O)C1 LTMHDMANZUZIPE-AMTYYWEZSA-N 0.000 description 7
- 229960005156 digoxin Drugs 0.000 description 7
- LTMHDMANZUZIPE-PUGKRICDSA-N digoxin Chemical compound C1[C@H](O)[C@H](O)[C@@H](C)O[C@H]1O[C@@H]1[C@@H](C)O[C@@H](O[C@@H]2[C@H](O[C@@H](O[C@@H]3C[C@@H]4[C@]([C@@H]5[C@H]([C@]6(CC[C@@H]([C@@]6(C)[C@H](O)C5)C=5COC(=O)C=5)O)CC4)(C)CC3)C[C@@H]2O)C)C[C@@H]1O LTMHDMANZUZIPE-PUGKRICDSA-N 0.000 description 7
- 150000001875 compounds Chemical class 0.000 description 6
- 229940082657 digitalis glycosides Drugs 0.000 description 5
- 125000005498 phthalate group Chemical group 0.000 description 5
- 210000004051 gastric juice Anatomy 0.000 description 4
- 229940079593 drug Drugs 0.000 description 3
- 239000003814 drug Substances 0.000 description 3
- 230000000694 effects Effects 0.000 description 3
- 235000011389 fruit/vegetable juice Nutrition 0.000 description 3
- 230000000968 intestinal effect Effects 0.000 description 3
- 239000000243 solution Substances 0.000 description 3
- 238000013268 sustained release Methods 0.000 description 3
- QZCLKYGREBVARF-UHFFFAOYSA-N Acetyl tributyl citrate Chemical compound CCCCOC(=O)CC(C(=O)OCCCC)(OC(C)=O)CC(=O)OCCCC QZCLKYGREBVARF-UHFFFAOYSA-N 0.000 description 2
- 208000020446 Cardiac disease Diseases 0.000 description 2
- WDJUZGPOPHTGOT-OAXVISGBSA-N Digitoxin Natural products O([C@H]1[C@@H](C)O[C@@H](O[C@@H]2C[C@@H]3[C@@](C)([C@@H]4[C@H]([C@]5(O)[C@@](C)([C@H](C6=CC(=O)OC6)CC5)CC4)CC3)CC2)C[C@H]1O)[C@H]1O[C@@H](C)[C@H](O[C@H]2O[C@@H](C)[C@@H](O)[C@@H](O)C2)[C@@H](O)C1 WDJUZGPOPHTGOT-OAXVISGBSA-N 0.000 description 2
- 229920003137 Eudragit® S polymer Polymers 0.000 description 2
- JAYAGJDXJIDEKI-PTGWOZRBSA-N Lanatoside C Chemical compound O([C@H]1[C@@H](OC(C)=O)C[C@@H](O[C@@H]1C)O[C@H]1[C@@H](O)C[C@@H](O[C@@H]1C)O[C@H]1[C@@H](O)C[C@@H](O[C@@H]1C)O[C@@H]1C[C@@H]2[C@]([C@@H]3[C@H]([C@]4(CC[C@@H]([C@@]4(C)[C@H](O)C3)C=3COC(=O)C=3)O)CC2)(C)CC1)[C@@H]1O[C@H](CO)[C@@H](O)[C@H](O)[C@H]1O JAYAGJDXJIDEKI-PTGWOZRBSA-N 0.000 description 2
- JAYAGJDXJIDEKI-UHFFFAOYSA-N Lanatoside C Natural products CC1OC(OC2CC3C(C4C(C5(CCC(C5(C)C(O)C4)C=4COC(=O)C=4)O)CC3)(C)CC2)CC(O)C1OC(OC1C)CC(O)C1OC(OC1C)CC(OC(C)=O)C1OC1OC(CO)C(O)C(O)C1O JAYAGJDXJIDEKI-UHFFFAOYSA-N 0.000 description 2
- MYEJFUXQJGHEQK-ALRJYLEOSA-N Proscillaridin Chemical compound O[C@@H]1[C@H](O)[C@@H](O)[C@H](C)O[C@H]1O[C@@H]1C=C2CC[C@H]3[C@@]4(O)CC[C@H](C5=COC(=O)C=C5)[C@@]4(C)CC[C@@H]3[C@@]2(C)CC1 MYEJFUXQJGHEQK-ALRJYLEOSA-N 0.000 description 2
- 229920002472 Starch Polymers 0.000 description 2
- 206010003119 arrhythmia Diseases 0.000 description 2
- 239000000872 buffer Substances 0.000 description 2
- 239000007931 coated granule Substances 0.000 description 2
- 238000000354 decomposition reaction Methods 0.000 description 2
- 229960000648 digitoxin Drugs 0.000 description 2
- WDJUZGPOPHTGOT-XUDUSOBPSA-N digitoxin Chemical compound C1[C@H](O)[C@H](O)[C@@H](C)O[C@H]1O[C@@H]1[C@@H](C)O[C@@H](O[C@@H]2[C@H](O[C@@H](O[C@@H]3C[C@@H]4[C@]([C@@H]5[C@H]([C@]6(CC[C@@H]([C@@]6(C)CC5)C=5COC(=O)C=5)O)CC4)(C)CC3)C[C@@H]2O)C)C[C@@H]1O WDJUZGPOPHTGOT-XUDUSOBPSA-N 0.000 description 2
- 239000002702 enteric coating Substances 0.000 description 2
- 238000009505 enteric coating Methods 0.000 description 2
- 208000019622 heart disease Diseases 0.000 description 2
- 229920003088 hydroxypropyl methyl cellulose Polymers 0.000 description 2
- 230000001771 impaired effect Effects 0.000 description 2
- 238000000338 in vitro Methods 0.000 description 2
- 238000001727 in vivo Methods 0.000 description 2
- 229960002614 lanatoside c Drugs 0.000 description 2
- 239000008363 phosphate buffer Substances 0.000 description 2
- 230000036470 plasma concentration Effects 0.000 description 2
- 229920002689 polyvinyl acetate Polymers 0.000 description 2
- 239000011118 polyvinyl acetate Substances 0.000 description 2
- 229930190098 proscillaridin Natural products 0.000 description 2
- 229960003584 proscillaridin Drugs 0.000 description 2
- MYEJFUXQJGHEQK-UHFFFAOYSA-N proscillaridin A Natural products OC1C(O)C(O)C(C)OC1OC1C=C2CCC3C4(O)CCC(C5=COC(=O)C=C5)C4(C)CCC3C2(C)CC1 MYEJFUXQJGHEQK-UHFFFAOYSA-N 0.000 description 2
- 239000002904 solvent Substances 0.000 description 2
- 239000008107 starch Substances 0.000 description 2
- 235000019698 starch Nutrition 0.000 description 2
- 239000000126 substance Substances 0.000 description 2
- 235000000346 sugar Nutrition 0.000 description 2
- 239000012730 sustained-release form Substances 0.000 description 2
- 230000001225 therapeutic effect Effects 0.000 description 2
- GUBGYTABKSRVRQ-XLOQQCSPSA-N Alpha-Lactose Chemical compound O[C@@H]1[C@@H](O)[C@@H](O)[C@@H](CO)O[C@H]1O[C@@H]1[C@@H](CO)O[C@H](O)[C@H](O)[C@H]1O GUBGYTABKSRVRQ-XLOQQCSPSA-N 0.000 description 1
- 229920003136 Eudragit® L polymer Polymers 0.000 description 1
- 229920003141 Eudragit® S 100 Polymers 0.000 description 1
- 206010019280 Heart failures Diseases 0.000 description 1
- 241000124008 Mammalia Species 0.000 description 1
- CERQOIWHTDAKMF-UHFFFAOYSA-N Methacrylic acid Chemical compound CC(=C)C(O)=O CERQOIWHTDAKMF-UHFFFAOYSA-N 0.000 description 1
- 229920000168 Microcrystalline cellulose Polymers 0.000 description 1
- 206010028813 Nausea Diseases 0.000 description 1
- 229920002125 Sokalan® Polymers 0.000 description 1
- 235000021355 Stearic acid Nutrition 0.000 description 1
- JDYLJSDIEBHXPO-ALNZGLKXSA-N [(2r,3r,4s,6r)-3-[(2s,4s,5r,6r)-4-acetyloxy-5-[(2s,4s,5r,6r)-4,5-diacetyloxy-6-methyloxan-2-yl]oxy-6-methyloxan-2-yl]oxy-6-[[(3s,5r,8r,9s,10s,13r,14s,16s,17r)-16-acetyloxy-14-hydroxy-10,13-dimethyl-17-(5-oxo-2h-furan-3-yl)-1,2,3,4,5,6,7,8,9,11,12,15,16,17 Chemical compound O([C@H]1[C@@H](OC(C)=O)C[C@@H](O[C@@H]1C)O[C@H]1[C@@H](OC(C)=O)C[C@@H](O[C@@H]1C)O[C@@H]1C[C@@H]2[C@]([C@@H]3[C@H]([C@]4(C[C@@H]([C@@H]([C@@]4(C)CC3)C=3COC(=O)C=3)OC(C)=O)O)CC2)(C)CC1)[C@H]1C[C@H](OC(C)=O)[C@H](OC(C)=O)[C@@H](C)O1 JDYLJSDIEBHXPO-ALNZGLKXSA-N 0.000 description 1
- 229940081735 acetylcellulose Drugs 0.000 description 1
- 229960003304 acetyldigoxin Drugs 0.000 description 1
- HWKJSYYYURVNQU-DXJNJSHLSA-N acetyldigoxin Chemical compound C1[C@H](OC(C)=O)[C@H](O)[C@@H](C)O[C@H]1O[C@@H]1[C@@H](C)O[C@@H](O[C@@H]2[C@H](O[C@@H](O[C@@H]3C[C@@H]4[C@]([C@@H]5[C@H]([C@]6(CC[C@@H]([C@@]6(C)[C@H](O)C5)C=5COC(=O)C=5)O)CC4)(C)CC3)C[C@@H]2O)C)C[C@@H]1O HWKJSYYYURVNQU-DXJNJSHLSA-N 0.000 description 1
- 239000013543 active substance Substances 0.000 description 1
- ACLJAFRNPZVVIW-ADFGDECNSA-N actodigin Chemical compound O([C@@H]1C[C@H]2CC[C@@H]3[C@@H]([C@]2(CC1)C)CC[C@]1([C@]3(O)CC[C@@H]1C=1C(OCC=1)=O)C)[C@@H]1O[C@H](CO)[C@@H](O)[C@H](O)[C@H]1O ACLJAFRNPZVVIW-ADFGDECNSA-N 0.000 description 1
- 229950004735 actodigin Drugs 0.000 description 1
- 239000000654 additive Substances 0.000 description 1
- 150000001298 alcohols Chemical class 0.000 description 1
- MGVYFNHJWXJYBE-UHFFFAOYSA-N alpha-Acetyl-digoxin Natural products CC1OC(CC(O)C1O)OC2C(O)CC(OC3C(C)OC(CC3OC(=O)C)OC4CCC5(C)C(CCC6C5CCC7(C)C(C(O)CC67O)C8=CC(=O)OC8)C4)OC2C MGVYFNHJWXJYBE-UHFFFAOYSA-N 0.000 description 1
- 229960004977 anhydrous lactose Drugs 0.000 description 1
- 239000012736 aqueous medium Substances 0.000 description 1
- 230000004071 biological effect Effects 0.000 description 1
- 229960000074 biopharmaceutical Drugs 0.000 description 1
- 230000015572 biosynthetic process Effects 0.000 description 1
- 239000007853 buffer solution Substances 0.000 description 1
- 239000002775 capsule Substances 0.000 description 1
- 229920002301 cellulose acetate Polymers 0.000 description 1
- 150000008280 chlorinated hydrocarbons Chemical class 0.000 description 1
- KRKNYBCHXYNGOX-UHFFFAOYSA-N citric acid Chemical class OC(=O)CC(O)(C(O)=O)CC(O)=O KRKNYBCHXYNGOX-UHFFFAOYSA-N 0.000 description 1
- 238000013270 controlled release Methods 0.000 description 1
- 239000003405 delayed action preparation Substances 0.000 description 1
- 230000001419 dependent effect Effects 0.000 description 1
- BLEBFDYUDVZRFG-UHFFFAOYSA-N dichloromethane;propan-2-ol Chemical compound ClCCl.CC(C)O BLEBFDYUDVZRFG-UHFFFAOYSA-N 0.000 description 1
- 125000004177 diethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 description 1
- 150000002148 esters Chemical class 0.000 description 1
- 150000002191 fatty alcohols Chemical class 0.000 description 1
- 230000002496 gastric effect Effects 0.000 description 1
- 239000007903 gelatin capsule Substances 0.000 description 1
- 229930182470 glycoside Natural products 0.000 description 1
- 150000002338 glycosides Chemical class 0.000 description 1
- 229930195733 hydrocarbon Natural products 0.000 description 1
- 150000002430 hydrocarbons Chemical class 0.000 description 1
- 230000007062 hydrolysis Effects 0.000 description 1
- 238000006460 hydrolysis reaction Methods 0.000 description 1
- 239000001866 hydroxypropyl methyl cellulose Substances 0.000 description 1
- 235000010979 hydroxypropyl methyl cellulose Nutrition 0.000 description 1
- 239000007788 liquid Substances 0.000 description 1
- 239000002609 medium Substances 0.000 description 1
- 229920003145 methacrylic acid copolymer Polymers 0.000 description 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 description 1
- IQSHMXAZFHORGY-UHFFFAOYSA-N methyl prop-2-enoate;2-methylprop-2-enoic acid Chemical compound COC(=O)C=C.CC(=C)C(O)=O IQSHMXAZFHORGY-UHFFFAOYSA-N 0.000 description 1
- -1 methylprocillaridin Chemical compound 0.000 description 1
- 229960003746 metildigoxin Drugs 0.000 description 1
- IYJMSDVSVHDVGT-PEQKVOOWSA-N metildigoxin Chemical compound O1[C@H](C)[C@@H](OC)[C@@H](O)C[C@@H]1O[C@@H]1[C@@H](C)O[C@@H](O[C@@H]2[C@H](O[C@@H](O[C@@H]3C[C@@H]4[C@]([C@@H]5[C@H]([C@]6(CC[C@@H]([C@@]6(C)[C@H](O)C5)C=5COC(=O)C=5)O)CC4)(C)CC3)C[C@@H]2O)C)C[C@@H]1O IYJMSDVSVHDVGT-PEQKVOOWSA-N 0.000 description 1
- 235000019813 microcrystalline cellulose Nutrition 0.000 description 1
- 239000008108 microcrystalline cellulose Substances 0.000 description 1
- 229940016286 microcrystalline cellulose Drugs 0.000 description 1
- 230000008693 nausea Effects 0.000 description 1
- QIQXTHQIDYTFRH-UHFFFAOYSA-N octadecanoic acid Chemical compound CCCCCCCCCCCCCCCCCC(O)=O QIQXTHQIDYTFRH-UHFFFAOYSA-N 0.000 description 1
- OQCDKBAXFALNLD-UHFFFAOYSA-N octadecanoic acid Natural products CCCCCCCC(C)CCCCCCCCC(O)=O OQCDKBAXFALNLD-UHFFFAOYSA-N 0.000 description 1
- 239000003960 organic solvent Substances 0.000 description 1
- 239000004014 plasticizer Substances 0.000 description 1
- 210000000813 small intestine Anatomy 0.000 description 1
- 239000008117 stearic acid Substances 0.000 description 1
- 230000002459 sustained effect Effects 0.000 description 1
- 231100000331 toxic Toxicity 0.000 description 1
- 230000002588 toxic effect Effects 0.000 description 1
- 239000001993 wax Substances 0.000 description 1
Landscapes
- Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- Epidemiology (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Biomedical Technology (AREA)
- Hematology (AREA)
- Heart & Thoracic Surgery (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Environmental & Geological Engineering (AREA)
- Anesthesiology (AREA)
- Vascular Medicine (AREA)
- Medicinal Preparation (AREA)
- Molecular Biology (AREA)
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| SE7813245A SE426548B (sv) | 1978-12-05 | 1978-12-22 | Fast farmaceutisk beredning innehallande en terapeutiskt effektiv hjertglykosid och en polymer |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| IE792455L IE792455L (en) | 1980-06-22 |
| IE48717B1 true IE48717B1 (en) | 1985-05-01 |
Family
ID=20336688
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| IE245579A IE48717B1 (en) | 1978-12-22 | 1979-12-18 | A pharmaceutical preparation comprising a cardiac glycoside in combination with a polymer,and a process for preparation thereof |
Country Status (7)
| Country | Link |
|---|---|
| DE (1) | DE2966037D1 (da) |
| ES (1) | ES8101888A1 (da) |
| FI (1) | FI794006A7 (da) |
| GR (1) | GR74016B (da) |
| IE (1) | IE48717B1 (da) |
| NO (1) | NO152634C (da) |
| PT (1) | PT70618A (da) |
-
1979
- 1979-12-13 DE DE7979850111T patent/DE2966037D1/de not_active Expired
- 1979-12-18 IE IE245579A patent/IE48717B1/en unknown
- 1979-12-20 FI FI794006A patent/FI794006A7/fi not_active Application Discontinuation
- 1979-12-20 PT PT7061879A patent/PT70618A/pt unknown
- 1979-12-21 NO NO794251A patent/NO152634C/no unknown
- 1979-12-21 ES ES487182A patent/ES8101888A1/es not_active Expired
- 1979-12-21 GR GR60840A patent/GR74016B/el unknown
Also Published As
| Publication number | Publication date |
|---|---|
| PT70618A (en) | 1980-01-01 |
| FI794006A7 (fi) | 1981-01-01 |
| IE792455L (en) | 1980-06-22 |
| DE2966037D1 (en) | 1983-09-08 |
| ES487182A0 (es) | 1980-12-16 |
| NO152634C (no) | 1985-10-30 |
| NO794251L (no) | 1980-06-24 |
| ES8101888A1 (es) | 1980-12-16 |
| GR74016B (da) | 1984-06-06 |
| NO152634B (no) | 1985-07-22 |
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